CACA [Ligand Id: 4148] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL32307 (Cis-4-Aminocrotonic Acid)
  • GABAA receptor ρ1 subunit/GABA receptor rho-1 subunit in Human [ChEMBL: CHEMBL3561] [GtoPdb: 420] [UniProtKB: P24046]
  • GABAA receptor ρ1 subunit in Rat [GtoPdb: 420] [UniProtKB: P50572]
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  • GABAA receptor ρ2 subunit/GABA receptor rho-2 subunit in Human [ChEMBL: CHEMBL2375] [GtoPdb: 421] [UniProtKB: P28476]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
GABAA receptor ρ1 subunit/GABA receptor rho-1 subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3561] [GtoPdb: 420] [UniProtKB: P24046]
ChEMBL Partial agonist activity against human rho1 subunit GABA-C receptor expressed in Xenopus oocytes F 4.13 pEC50 74000 nM EC50 J Med Chem (2000) 43: 1427-1447 [PMID:10780899]
ChEMBL Agonist activity at human GABAc Rho1 receptor expressed in Xenopus oocytes assessed as whole cell current production by two electrode voltage clamp method F 4.13 pEC50 74000 nM EC50 J Med Chem (2008) 51: 3825-3840 [PMID:18528996]
GABAA receptor ρ1 subunit in Rat [GtoPdb: 420] [UniProtKB: P50572]
GtoPdb - - 4.13 pEC50 74000 nM EC50 Mol Pharmacol (1993) 43: 609-25 [PMID:8386310]
GABAA receptor ρ2 subunit/GABA receptor rho-2 subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2375] [GtoPdb: 421] [UniProtKB: P28476]
ChEMBL Partial agonist activity against human rho-2 subunit GABA-C receptor expressed in Xenopus oocytes F 4.15 pEC50 70000 nM EC50 J Med Chem (2000) 43: 1427-1447 [PMID:10780899]

ChEMBL data shown on this page come from version 33:

Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]